解毒抗癌巴布剂中主要成分体外释放度及离体小鼠经皮渗透行为研究

In Vitro Release and Percutaneous Osmotic Behavior in Mice Major Components in Detoxifying Anti-cancer Cataplasm

目的对解毒抗癌巴布剂中主要成分栀子苷、芍药苷、橙皮苷的释放度及离体小鼠透皮率测定研究。方法采用改良的France扩散池,以离体小鼠皮模拟人皮肤屏障,采用高效液相色谱(HPLC)法分别测定其有效成分。结果解毒抗癌巴布剂中栀子苷在10,30,60,90,120 min的累积释放度分别为12.75%,39.27%,48.76%,67.84%,83.81%。芍药苷的累积释放度分别为14.36%,37.55%,52.10%,66.88%,84.17%;橙皮苷的累积释放度分别为10.27%,36.74%,49.10%,58.22%,79.38%。解毒抗癌巴布剂中栀子苷、芍药苷、橙皮苷透过离体小鼠皮肤24 h的透皮率分别为26.55%,23.64%,29.16%。结论解毒抗癌巴布剂的小鼠体外经皮渗透行为以Higuchi方程拟合为优,拟合度最高,表明解毒抗癌巴布剂为骨架型控释制剂。

Objective To study the release of geniposide,paeoniflorins and hesperidin in anti-cancer cataplasm and determine the transdermal rate of isolated mice in vitro.Methods The modified France diffusion cell was used to simulate the human skin barrier with isolated mouse skin in vitro.The effective components were determined by the HPLC method.Results The cumulative releaserates of geniposide in the cataplasm at 10,30,60,90 and 120 min were 12.75%,39.27%,48.76%,67.84%,and 83.81%,respectively.The cumulative releaserates of paeoniflorin were 14.36%,37.55%,52.10%,66.88%,and 84.17%respectively,and those of hesperidin were 10.27%,36.74%,49.10%,58.22%,and 79.38%,respectively.The transdermal rates of geniposide,paeoniflorin,and hesperidin through the skin of isolated mice for 24 hours in the detoxification anti-cancer cataplasm were 26.55%,23.64%,and 29.16%,respectively.Conclusion In vitro percutaneous osmotic behavior of detoxifying anti-cancer cataplasm in mice was optimized by Higuchi equation fitting,and the degree of fitting was the highest,indicating that the cataplasm was a skeleton controlled-release preparation.